CDK

Cat. No.

A54387

CAS No.

672324-11-7

CDK-IN-19

CDK-IN-19 is a potent cyclin-dependent kinase (CDK) inhibitor that selectively targets CDK enzymes involved in cell cycle regulation. This compound demonstrates significant antiproliferative activity and is valuable for cancer research applications, particularly in studying CDK-mediated pathways and the effects of cell cycle disruption in oncogenesis. Its role as a CDK inhibitor makes it a crucial tool for investigating therapeutic strategies aimed at cancer treatment.

Cat. No.

A54388

CAS No.

1366002-73-4

SNX2-1-108

SNX2-1-108 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8). This compound plays a pivotal role in modulating transcriptional regulation and is essential for various cellular processes. Its inhibition of CDK8 activity has significant implications in cancer research, particularly in studying the regulatory pathways of gene expression and potential therapeutic interventions in CDK8-dependent malignancies.

Cat. No.

A54389

CAS No.

2891574-93-7

EF-4-177

EF-4-177 is an allosteric inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 87 nM. This compound effectively interferes with spermatogenesis, making it a valuable tool for studying male reproductive biology and the regulatory mechanisms of cell cycle progression. Its oral activity enhances its utility in pharmacological research and potential therapeutic applications.

Cat. No.

A54390

CAS No.

2654003-68-4

SZ-015268

SZ-015268 is a potent CDK7 inhibitor, exhibiting an IC50 of 23.56 nM. This compound demonstrates significant anti-tumor activity, effectively inhibiting the proliferation of various cancer cell lines, including HCC70 (IC50 33 nM), OVCAR-3 (IC50 80.56 nM), HCT116 (IC50 12.53 nM), and HCC1806 (IC50 61.55 nM). SZ-015268 serves as a valuable tool in cancer research, particularly in studies focused on cell cycle regulation and therapeutic strategies targeting CDK7.

Cat. No.

A54391

CAS No.

2935587-91-8

PROTAC CDK9 degrader-6

PROTAC CDK9 degrader-6 is a proteolysis-targeting chimera (PROTAC) designed to specifically target and degrade cyclin-dependent kinase 9 (CDK9) through the ubiquitin-proteasome system. This compound effectively induces the degradation of CDK9, exhibiting DC50 values of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively. It is useful in research applications investigating the modulation of transcriptional regulation and the therapeutic potential in cancers driven by aberrant CDK9 activity.

Cat. No.

A54392

CAS No.

3020773-91-2

PROTAC CDK9/CycT1 Degrader-2

PROTAC CDK9/CycT1 Degrader-2 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 45 nM. This compound promotes targeted protein degradation, thereby modulating transcriptional regulation and influencing cellular processes associated with gene expression. It is valuable for research applications focused on cancer biology and therapeutic development by addressing dysregulated CDK9 activity.

Cat. No.

A54393

CAS No.

3036014-62-4

CDK4/6-IN-22

CDK4/6-IN-22 is a potent dual inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting these kinases, CDK4/6-IN-22 effectively disrupts cell cycle progression, making it a valuable tool in cancer research. This compound is particularly relevant for studies exploring therapeutic strategies for tumors characterized by dysregulated CDK4/6 activity.

Cat. No.

A54395

CAS No.

496864-14-3

Aloisine B

Aloisine B is a potent cyclin-dependent kinase (CDK) inhibitor. It effectively inhibits cell proliferation by inducing cell cycle arrest in both the G1 and G2 phases through competition for the ATP-binding pocket. This compound serves as a valuable tool for research in cancer biology and cell cycle regulation.

Cat. No.

A54397

CAS No.

3036231-62-3

Cyclin A/B RxL-IN-1

Cyclin A/B RxL-IN-1 is an inhibitor that targets the interaction between Cyclin A/B and the hydrophobic patch (HP). With an IC50 of 0.12 μM, it effectively inhibits Cyclin A, demonstrating notable antitumor activity in cell line-derived xenograft (CDX) models. This compound is valuable for research on E2F-driven cancers, including small-cell lung cancer (SCLC), providing insights into therapeutic strategies.

Cat. No.

A54399

CAS No.

247149-58-2

CDK2-IN-29

CDK2-IN-29 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 96 nM. Additionally, it shows activity against CDK4 with an IC50 of 360 nM. This compound is instrumental in the study of cell cycle regulation and has potential applications in cancer research, where CDK inhibition plays a critical role in controlling cell proliferation.

Cat. No.

A54400

CAS No.

2654003-64-0

CDK7-IN-8

CDK7-IN-8 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of 54.29 nM. This compound effectively inhibits the proliferation of specific cancer cell lines and has shown promising activity in various in vivo tumor models. CDK7-IN-8 is utilized in research applications targeting cancer therapeutics and cell cycle regulation studies.

Cat. No.

A54402

CAS No.

2606780-39-4

Cdc7-IN-19

Cdc7-IN-19 is a highly potent inhibitor of CDC7, exhibiting an IC50 of 1.49 nM. This compound disrupts the kinase activity of CDC7, playing a critical role in the regulation of DNA replication and cell cycle progression. It is valuable for studying the molecular mechanisms of cancer, particularly in the development of targeted therapies that influence cell proliferation.

Cat. No.

A54403

CAS No.

2765676-02-4

CDK7-IN-15

CDK7-IN-15 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative exhibits potent inhibitory activity, making it a valuable tool for investigating transcriptional dysregulation in various cancer types. CDK7-IN-15 is particularly relevant for cancer research focused on therapeutic strategies targeting aberrant transcriptional control.

Cat. No.

A54405

CAS No.

2821777-43-7

RLY-2139

Synonyms: CDK2-IN-26

RLY-2139 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2). By selectively targeting CDK2, it disrupts cell cycle progression, making it a valuable tool for studying cell division and proliferation. RLY-2139 has potential applications in cancer research, particularly in exploring therapeutic strategies for CDK2-related malignancies.

Cat. No.

A54406

CAS No.

1253647-46-9

rel-(2S,3R)-Voruciclib hydrochloride

rel-(2S,3R)-Voruciclib hydrochloride is the rel-(2S,3R)-enantiomer of Voruciclib, a potent inhibitor of cyclin-dependent kinases (CDKs). This compound exhibits significant biological activity in regulating cell cycle progression and has potential applications in cancer research, particularly in therapeutic strategies targeting CDK-mediated pathways. Its oral bioavailability makes it a valuable tool for in vivo studies of cell proliferation and tumor growth.

Cat. No.

A54407

CAS No.

3064485-73-7

Cyclin A/B RxL-IN-2

Cyclin A/B RxL-IN-2 is a macrocyclic peptide that acts as a selective inhibitor of Cyclin A and Cyclin B. It exhibits high potency with an IC50 of 0.05 μM for Cyclin A and less than 0.02 μM for Cyclin B, alongside Kd values of 2.7 nM and 1.0 nM, respectively. This compound competes for binding at the hydrophobic patch of Cyclin A/B, disrupting interactions with the substrate RxL motif, leading to replication stress and DNA damage in E2F-high cells, as well as inducing mitotic catastrophe and apoptosis. Cyclin A/B RxL-IN-2 demonstrates efficacy in inhibiting tumor growth in NCI-H69 and NCI-H446 small cell lung cancer xenograft models, making it a valuable tool for research in small-cell lung cancer.

Cat. No.

A54408

CAS No.

2789680-97-1

PRT3645

PRT3645 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). It demonstrates potent inhibition with IC50 values less than 20 nM, making it a valuable tool for studying cell cycle regulation and cancer biology. PRT3645 is primarily utilized in research applications targeting tumor cell proliferation and therapeutic strategies for cancers associated with dysregulated CDK4/6 activity.

Cat. No.

A54410

CAS No.

2606780-38-3

Cdc7-IN-8

Cdc7-IN-8 is a potent inhibitor of Cdc7, a serine/threonine kinase essential for the activation of the MCM protein, which plays a critical role in the initiation of DNA replication. By blocking Cdc7 activity, Cdc7-IN-8 exhibits significant potential in cancer research by disrupting DNA replication processes. This compound serves as a valuable tool for investigating the mechanisms of oncogenesis and evaluating therapeutic strategies targeting cell proliferation.

Cat. No.

A54411

CAS No.

1093294-48-4

GW780056X

GW780056X is a selective inhibitor of Cyclin-Dependent Kinase 12 (CDK12). It is known to reduce nuclear foci count in DM1 cells, demonstrating its potential in therapeutic strategies for myotonic dystrophy type 1. This compound serves as a valuable tool for investigating the molecular mechanisms underlying this genetic disorder and evaluating potential treatment options.

Cat. No.

A54412

CAS No.

642002-74-2

CDK8-IN-18

CDK8-IN-18 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 of 43 μM. This compound is instrumental in studying the regulatory roles of CDK8 in transcription and its implications in oncogenesis. CDK8-IN-18 is widely used in cancer research to explore the therapeutic potential of targeting CDK8 in malignancies.

Cat. No.

A54414

CAS No.

2747919-19-1

CDK7/9-IN-1

CDK7/9-IN-1 is a potent inhibitor of cyclin-dependent kinases 7 and 9, demonstrating a selective inhibition profile that favors CDK7. This compound exhibits IC50 values of 0.0656 μM and 0.00574 μM for CDK7 without and with 3 hours of pre-incubation, respectively, while inhibiting CDK9 with an IC50 of 2.14 μM after pre-incubation. CDK7/9-IN-1 is valuable for research applications related to cancer, particularly in studies targeting the regulation of transcription and cell cycle progression mediated by these kinases.

Cat. No.

A54415

CAS No.

3033863-94-1

CDK12-IN-7

CDK12-IN-7 is a potent inhibitor of cyclin-dependent kinases CDK12 and CDK2, exhibiting IC50 values of 42 nM and 196 nM, respectively. This compound demonstrates significant anti-cell proliferation activity, making it valuable for cancer research applications. Its selective inhibition of CDK12 may provide insights into tumorigenesis and potential therapeutic strategies in oncology.

Cat. No.

A54416

CAS No.

1335490-39-5

BAY-958

BAY-958 is a potent inhibitor of PTEFb/CDK9, demonstrating high selectivity within the cyclin-dependent kinase family. This compound exhibits significant antiproliferative effects against various cancer cell lines, including HeLa and MOLM-13. Additionally, BAY-958 shows favorable metabolic stability and effectively reduces tumor growth in mouse xenograft models while maintaining a low toxicity profile, making it a valuable tool for cancer research.

Cat. No.

A54417

CAS No.

3024545-79-4

CDK7-IN-26

CDK7-IN-26 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of 7.4 nM. This compound demonstrates significant efficacy in inhibiting the proliferation of triple-negative breast cancer (TNBC) cell line-derived xenograft tumors in vivo. In vitro studies show that CDK7-IN-26 effectively targets MDA-MB-453 cells, exhibiting an IC50 of 0.15 μM, making it a valuable tool for cancer research focusing on CDK7 inhibition.

Cat. No.

A54418

CAS No.

2651196-69-7

CDK12-IN-4

CDK12-IN-4 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a potent inhibitory effect with an IC50 of 0.641 μM at elevated ATP levels (2 mM). This compound demonstrates no significant activity against CDK2/Cyclin E or CDK9/Cyclin T1, with IC50 values exceeding 20 μM under the same conditions. CDK12-IN-4 is valuable for research into transcription regulation and therapeutic targeting in cancer biology, particularly in studies involving DNA damage and repair pathways.